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Sulfonylureas

Stimulate insulin production from the pancreas.

Lower blood glucose by stimulating the pancreas to increase the production and release of endogenous insulin.

Three sulfonylureas are available-glimepiride, glidpizide, and glyburide.

The sulfonylureas cell are roughly clinically interchangeable terms of hemoglobin A-1 C lowering.

Secondary effects include decreasing hepatic glucose production.

Sulfonylureas stimulate insulin release by closure of specific potassium channel on beta cells.

Sulfonylureas lead to reductions in hemoglobin A-1 C levels on the order of 1-2%.

Beneficial effects of sulfonylureas on Hgb A1C wanes with time.

May be associated with excess cardiovascular morbidity.

Adverse effects include weight gain, and risk for hypoglycemia,and uncertainty regarding their cardiovascular safety.

Effective in 50-60% of patients as initial therapy for type 2 diabetes, but are associated with long-term failure rate of 5-7% per year.

Suggested use may lead to more quick pancreas burnout.

Adverse effects include hypoglycemia, weight gain and hypersensitivity.

Hypoglycemia reported at a rate of 1.23 hospitalizations per hundred patients per year.

Sulfonylureas lead to most ED visits for hypoglycemia.

Glyburide is associated with an increased hypoglycemic risk compared to glipizide.

Glimepiride has the highest incidence of hypoglycemia of the three agents, and this may be due to its longer half-life, allowing for once daily dosing.

All 3 drugs undergo hepatic metabolism with glyburide having active metabolites, the key difference from other drugs.

Glyburide and glpizide require twice daily administration because of their shorter half life.

Hypoglycemia is associated with significant morbidity including impaired cognition function, higher risk of dementia, stroke, and death.

Sulfonylurea monotherapy is associated with a higher risk of all-cause mortality, major hypoglycemic episodes, and cardiovascular events compared with Metformin (Whitlock RH).

Sulfonylureas associated with hypoglycemia, and this problem is enhanced by the use of concomitant amntibiotics such as clarithromycin levofloxacin, sulfamethoxazole-trimethoprim, metronidazole, and ciprofloxacin.

 

Sulfonylurea monotherapy is associated with a higher risk of all cause mortality, major hypoglycemic episodes and cardiovascular events compared with Metformin.

 

 

 

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